Clarinex-D 12 Hour (desloratadine/pseudoephedrine sulfate)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Desloratadine, the active descarboethoxy metabolite of loratadine, is a second generation antihistamine.
Pseudoephedrine is a sympathomimetic agent that occurs naturally in plants of the genus Ephedra; the drug acts directly on both alpha- and, to a lesser degree, beta-adrenergic receptors.
Desloratadine, the active descarboethoxy metabolite of loratadine, is a long-acting tricyclic antihistamine. The drug has been characterized as a specific, selective peripheral H1-receptor antagonist. Experimental evidence indicates that desloratadine also suppresses the release of histamine from human mast cells.
Because desloratadine does not readily cross the blood-brain barrier, the drug has been referred to as a relatively ''nonsedating'' or second generation antihistamine.
Desloratadine is commercially available for oral administration as conventional tablets, orally disintegrating tablets, oral solution, and as an extended-release tablet containing desloratadine in fixed combination with pseudoephedrine sulfate. Desloratadine orally disintegrating tablets recently have been reformulated to improve palatability.
Following oral administration of desloratadine 5 mg once daily for 10 days as conventional tablets, peak plasma concentrations of the drug were achieved in approximately 3 hours. Following oral administration of a single 5-mg dose of desloratadine as a fixed-combination, extended-release tablet also containing pseudoephedrine sulfate, peak plasma concentrations of desloratadine were achieved in approximately 6-7 hours. Food or grapefruit juice does not appear to affect bioavailability of desloratadine following administration as conventional tablets, oral solution, or extended-release fixed-combination tablets; water does not appear to affect bioavailability of desloratadine following administration as orally disintegrating tablets.
The manufacturer states that desloratadine conventional tablets and oral solution are bioequivalent. The currently available reformulated orally disintegrating tablets containing 5 mg of desloratadine are bioequivalent to the original orally disintegrating formulation (no longer commercially available), which previously was shown to be bioequivalent to desloratadine conventional tablets and oral solution. The extended-release fixed-combination tablets are not bioequivalent with desloratadine conventional tablets.
Following oral administration of the fixed-combination preparation containing 5 mg of desloratadine and 240 mg of pseudoephedrine sulfate, plasma concentrations of desloratadine and 3-hydroxydesloratadine were 15-20% lower than those achieved with the 5-mg conventional tablets.
Following single- and multiple-dose administration, antihistaminic effects of desloratadine occur within 1 hour and persist for up to 24 hours. There is no evidence of histamine-induced skin wheal tachyphylaxis following 28 days of treatment with desloratadine 5 mg daily; the clinical relevance of histamine wheal skin testing has not been established.
Desloratadine is extensively metabolized to 3-hydroxydesloratadine, an active metabolite that subsequently undergoes glucuronidation; the enzyme(s) responsible for metabolism of desloratadine has not been identified. Data from clinical trials and pharmacokinetic studies indicate that approximately 6% of patients receiving desloratadine exhibit a decreased ability to form 3-hydroxydesloratadine and, therefore, are classified as poor metabolizers of the drug; the frequency of poor metabolizers appears to be higher in blacks (17%) than in Caucasians (2%) or Hispanics (2%). Poor metabolizers experience a substantially (approximately sixfold) greater exposure to desloratadine than normal metabolizers; however, no overall differences in safety were observed between these groups.
Nevertheless, the manufacturer states that an increased risk of adverse effects in poor metabolizers cannot be ruled out.
Approximately 87% of a radiolabeled oral dose of desloratadine is excreted as metabolic products in urine and feces in equal proportions.
Desloratadine, an active metabolite of loratadine, is used for the management of allergic rhinitis and chronic idiopathic urticaria. The drug also has been used in patients with seasonal allergic rhinitis who have concomitant mild to moderate asthma. For additional information on these and other uses of antihistamines, see Uses in the Antihistamines General Statement 4:00.
Generic name: desloratadine/pseudoephedrine sulfate
Pronunciation: (des-lor-AT-uh-deen/sue-doh-eff-ED-rin)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Clarinex-D 12 Hour
Indications
The following indications are listed for Clarinex-D 12 Hour:
- Seasonal Allergic Rhinitis
Also known as: Intermittent Allergic Rhinitis, Periodic Runny Nose, Seasonal Allergy.
Dosing
No dosing information is available for this tab.
Desloratadine is administered orally once daily without regard to meals.
Desloratadine orally disintegrating tablets are administered by placing a tablet on the tongue, allowing it to disintegrate, and then subsequently swallowing with or without water. Patients receiving desloratadine orally disintegrating tablets should be instructed not to remove a tablet from the blister until just prior to dosing. Desloratadine oral solution should be administered using a commercially available dropper or syringe that is calibrated to deliver 2 or 2.5 mL. Extended-release tablets containing desloratadine in fixed combination with pseudoephedrine sulfate should be swallowed intact and should not be chewed, broken, or crushed.
Commercially available desloratadine conventional tablets and oral solution are bioequivalent. The currently available reformulated orally disintegrating tablets containing 5 mg of desloratadine are bioequivalent to the original orally disintegrating formulation (no longer commercially available), which previously was shown to be bioequivalent to desloratadine conventional tablets and oral solution.
Pseudoephedrine hydrochloride and sulfate are administered orally.
Pseudoephedrine hydrochloride 240-mg extended-release tablets should be administered orally once daily and swallowed whole with water; the extended-release tablets should not be divided, crushed, chewed, or dissolved. Patients should be advised that the tablet does not completely dissolve and may be passed in the stool.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
No formal drug interaction studies have been performed with the fixed-combination preparation containing desloratadine and pseudoephedrine sulfate. When using this preparation, consider the drug interactions associated with pseudoephedrine (e.g., monoamine oxidase (MAO) inhibitors).
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Known hypersensitivity to desloratadine, loratadine, or any ingredient in the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects reported in 2% or more of patients 12 years of age and older receiving desloratadine for management of allergic rhinitis and occurring more frequently than placebo include pharyngitis, dry mouth, myalgia, fatigue, somnolence, and dysmenorrhea. Adverse effects reported in at least 2% of patients 12 years of age and older receiving desloratadine for management of chronic idiopathic urticaria and more frequently than placebo include headache, nausea, fatigue, dizziness, pharyngitis, dyspepsia, and myalgia.
Adverse effects reported in 2% or more of pediatric patients (2-5 years of age) receiving desloratadine and occurring more frequently than placebo include fever, urinary tract infection, and varicella (chicken pox). Adverse effects reported in 2% or more of patients 12-23 months of age and occurring more frequently than placebo include fever, diarrhea, upper respiratory tract infection, coughing, increased appetite, emotional lability, epistaxis, parasitic infection, pharyngitis, and maculopapular rash. Adverse effects reported in 2% or more of patients 6-11 months of age and occurring more frequently than placebo include upper respiratory tract infection, diarrhea, fever, irritability, coughing, somnolence, bronchitis, otitis media, vomiting, anorexia, pharyngitis, insomnia, rhinorrhea, erythema, and nausea.
Adverse effects reported in 2% or more of patients 12 years of age and older receiving the fixed combination of desloratadine and pseudoephedrine sulfate include dry mouth, headache, insomnia, fatigue, pharyngitis, somnolence, nausea, dizziness, nervousness, hyperactivity, and anorexia.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy have not been established for symptomatic management of seasonal allergic rhinitis in children younger than 2 years of age.
Safety and efficacy have not been established for symptomatic management of perennial allergic rhinitis or chronic idiopathic urticaria in children younger than 6 months of age.
Safety and efficacy of the fixed-combination preparation containing desloratadine and pseudoephedrine sulfate for symptomatic management of seasonal allergic rhinitis have not been established in children younger than 12 years of age.
Overdosage and toxicity (including death) have been reported in children younger than 2 years of age receiving nonprescription (over-the-counter, OTC) preparations containing antihistamines, cough suppressants, expectorants, and nasal decongestants alone or in combination for relief of symptoms of upper respiratory tract infection. Clinicians should ask caregivers about use of nonprescription cough and cold preparations to avoid overdosage. For additional information on precautions associated with the use of cough and cold preparations in pediatric patients, see Cautions: Pediatric Precautions in the Antihistamines General Statement 4:00.
Category C. (See Users Guide.)
Desloratadine is distributed into milk. Discontinue nursing or the drug, taking into account the importance of the drug to the woman. Exercise caution if the fixed-combination preparation containing desloratadine and pseudoephedrine sulfate is used in nursing women.
Experience with desloratadine in those 65 years of age and older is insufficient to determine whether they respond differently from younger adults. In one study, peak plasma concentrations and area under the plasma concentration-time curve (AUC) of desloratadine were increased (by 20%) and plasma elimination half-life was prolonged in geriatric patients compared with younger adults; however, these age-related differences do not appear to be clinically important. Nevertheless, dosage should be selected with caution because of the greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy observed in geriatric patients.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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